Small inhibitors of ADP-ribosylation factor activation and function in mammalian cells

Table 1 Targets and effects of the ADP-ribosylation factor inhibitors

Inhibitor	Arf regulators	Arf	Phenotype/function	Cell type
Brefeldin A	GBF1	Arf1	Tubulation and collapse of Golgi apparatus	Mammalian cells
	Gea1p/2p	Arf5
	Sec7p	Arf1p	Inhibition of protein secretion	Yeast
LM11	Cytohesin-2	Arf1	Dispersion of Golgi markers	MDCK cells
	BIG1	Arf5	Inhibition of migration
Golgicide A	GBF1	Arf1	Protection from Shiga toxin toxicity	Mammalian cells
			Dispersion of cis- and medial-Golgi
			Inhibition of protein secretion
			Inhibition of viral replication: (hepatitis C virus; enteroviruses; poliovirus; coxsackievirus)
EXO1	ArfGAPs	Arf1	Tubulation, collapse of Golgi	Mammalian cells
EXO2	BIG1	Arf1	Dispersion of the trans-Golgi network	HeLa cells
			Interfere with shiga toxin trafficking to the endoplasmic reticulum
LG186	BIG1	Arf1	Dissociation of COP I vesicles from the Golgi	HeLa cells
	GBF1
M69 aptamer	Cytohesin-1	Arf1	Actin remodelling	Jurkat T cells
	Cytohesin-2		Inhibition of adhesion
K61 aptamer	Cytohesin-1	Arf1	Inhibition of serum-induced ERK MAP Kinase activation	HeLa cells
	Cytohesin-2
SecinH3	Cytohesin-1	Arf1	Insulin resistance	HepG2 cells; rat and human β pancreatic cells
	Cytohesin-2	Arf6
	Cytohesin-3		Inhibition of superoxide anion production	Neutrophils
			Inhibition of degranulation
			Activation of Mac-1-dependent adhesion, phagocytosis and migration
			Inhibition of LFA-1 dependent adhesion
			Inhibition of migration	3T3-L1 cells
			Inhibition of neuritis outgrowth	N1E-115 neublastoma cells
			Regulation of β-1 integrin internalization and of β-1 integrin-dependent adhesion	HeLa cells
	Steppke		Insulin resistance	Fly cells

Arf: ADP-ribosylation factor; GBF: Golgi-specific Brefeldin A-resistance factor; BIG: Brefeldin A-inhibited GEF.